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IOX1

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Chemical Structure| 5852-78-8 同义名 : 5-羰基-8-羟基喹啉
CAS号 : 5852-78-8
货号 : A170634
分子式 : C10H7NO3
纯度 : 99%
分子量 : 189.167
MDL号 : MFCD18417145
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(63.44 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • KDM2

    KDM2A, IC50:1.8 μM

  • KDM4

    KDM4E, IC50:2.3 μM

    KDM4C, IC50:0.6 μM

  • KDM6

    KDM6B, IC50:1.6 μM

  • KDM5

    KDM5C, IC50:19 μM

  • KDM3

    KDM3A, IC50:0.1 μM
描述 The Jumonji C domain (JmjC) demethylases belong to the superfamily of FeII and 2-oxoglutarate (2OG) oxygenases. IOX1 is a potent inhibitor against a broad-spectrum of 2OG oxygenases, including non-JmjC 2OG oxygenases, with in vitro IC50 values in the micromolar range. Treatment of HeLa cells with 300μM of IOX1 led to a dose-dependent increase in H3K9me3 fluorescence intensity compared to the DMSO-treated control group. The cellular EC50 value of IOX1 in HeLa cells was 100μM. The amplified luminescent proximity homogeneous assay revealed that the IC50 value of IOX1 for the inhibition of H3K9me3 demethylation activity of isolated KDM4C was 0.6μM. The IC50 values of IOX1 for KDM4E, KDM2A, KDM3A, KDM5C, KDM6B, and PHD2 were 2.3, 1.8, 0.1, 19.0, 1.4, and 33.0μM, respectively.[3] In immunocompetent C57BL/6 mice harboring B16F10 tumors with a volume of about 50 mm3, repetitive intraperitoneal administration of IOX1 (2.5mg/kg) every two days significantly attenuated melanoma expansion at 10 days after treatment.[4]
作用机制 IOX1 is a potent, broad-spectrum 2OG oxygenase inhibitor with low cell permeability due to its polar C-5 carboxyl group.[3]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HCT116 cells Cytotoxicity assay 48 h Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=28.1 μM 26491978
human A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=48.3 μM 26491978
human HeLa cells Function assay 72 h Induction of histone methylation in human HeLa cells assessed as H3K9me2 level after 72 hrs by immunofluorescence assay 24325601
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.29mL

1.06mL

0.53mL

26.43mL

5.29mL

2.64mL

52.86mL

10.57mL

5.29mL
参考文献

[1]Hu Q, Chen J, et al. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins. Int J Mol Med. 2016 Jan;37(1):189-96.

[2]Schiller R, Scozzafava G, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71.

[3]Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC, Mott BT, McCullagh JS, Maloney DJ, Schofield CJ, Kawamura A. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71

[4]Yu Y, Schleich K, Yue B, Ji S, Lohneis P, Kemper K, Silvis MR, Qutob N, van Rooijen E, Werner-Klein M, Li L, Dhawan D, Meierjohann S, Reimann M, Elkahloun A, Treitschke S, Dörken B, Speck C, Mallette FA, Zon LI, Holmen SL, Peeper DS, Samuels Y, Schmitt CA, Lee S. Targeting the Senescence-Overriding Cooperative Activity of Structurally Unrelated H3K9 Demethylases in Melanoma. Cancer Cell. 2018 Feb 12;33(2):322-336.e8